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Binding of FGFs to FGFRs leads to receptor dimerization
2021-12-10

Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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lumacaftor br Discussion Our results showed that the
2021-12-10

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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Taken together this study provides the proof of
2021-12-10

Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic
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GnRH receptor GnRH R levels are elevated
2021-12-09

GnRH receptor (GnRH-R) levels are elevated in decidualized stromal cells, suggesting a function for the GnRH–GnRH-R pathway in the early implantation events. Both GnRH and GnRH-R have been shown to be present in preimplantation embryos and the fallopian tubes at both mRNA and protein levels (). Two
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Extending the issue of the species differences the
2021-12-09

Extending the issue of the species differences, the role of neuroestradiol in the preovulatory GnRH/LH surge might be specific to primates or species with a luteal phase. For example, animals with a true luteal phase, such as monkeys and sheep, exhibit a long preovulatory GnRH surge, lasting well af
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Although side effects as paresthesia due
2021-12-09

Although side effects as paresthesia due to the application of β-alanine are known, a study in 2006 pointed out that there are no clinical (biochemical or hematological) changes after a long-term supplementation with β-alanine. In 2015, the International Society of Sports Nutrition rejected any argu
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br Materials and methods br Results br Discussion Neurotrans
2021-12-09

Materials and methods Results Discussion Neurotransmitter uptake is one of the most important aspects of synaptic transmission, it fact, the existence of a specific uptake system is one of the requisites that any neuroactive substance has to cover to be considered a neurotransmitter. It has
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In the latent inhibition model
2021-12-09

In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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br Mechanisms of gap junction internalization disaggregation
2021-12-09

Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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Cx mimetic peptides short synthetic peptides corresponding
2021-12-09

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino Galanthamine sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a conce
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YM 90709 An advantage of photolabeling with tritiated photop
2021-12-09

An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled YM 90709 and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with other lig
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Michiel S van der Heijden had full access to
2021-12-09

Michiel S. van der Heijden had full access to all L-161,982 data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang, Sustic,
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Compound a substituted phenyl H pyrano d d dipyrimidine
2021-12-09

Compound 6, a 5-(4-substituted-phenyl)-5H-pyrano[2,3-d:-6,5-d′]dipyrimidine derivative was invented previously to have significant efficacy to inhibit HIV integrase enzyme with 0.9 ± 0.4 μM of IC50 against 3′-processing and 16.1 ± 10.7 μM of IC50 against strand transfer suppression. The compound ind
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br Drugs approved or in development
2021-12-09

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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MK-3207 HCl receptor Due to the importance of gene regulatio
2021-12-08

Due to the importance of gene regulation in cancers, HDAC inhibitors have been studied extensively in cancer biology and are in current clinical use as anti-tumor therapies [17]. The HDAC inhibitors vorinostat, romidepsin, and belinostat have been approved for certain T-cell lymphomas, and panobinos
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